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We have applied our expertise in multivalency to discover product candidates and lead compounds in a number of therapeutic areas.
Oral Peripheral Mu Opioid Receptor Antagonist (PµMA)
Opioid analgesics such as morphine continue to play a critical role in chronic malignant and non-malignant pain control. Opioid-induced constipation (OIC) is a common and well recognized complication of opioid therapy that has a significant impact on the quality of life of patients. The abdominal discomfort and nausea associated with OIC can be debilitating and may interfere with successful pain management.
TD-1211 is a multivalent inhibitor of the mu opioid receptor that was discovered and developed by Theravance.
We demonstrated preclinically that TD-1211 is orally bioavailable with no evidence of activity in the CNS (in other words, TD-1211 is "peripherally restricted"). TD-1211 was designed as a once-daily treatment to alleviate gastrointestinal side effects of opioid analgesic therapy without affecting analgesia. The goal of this program is to identify and develop a best-in-class-treatment for OIC.
We have completed a Phase 2 study evaluating TD-1211 in patients experiencing OIC. The compound was generally well tolerated and reduced symptoms of constipation without interfering with analgesia.